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可注射奥沙利铂缓释微粒制备及其理化性质研究OA北大核心CSTPCD

Preparation and physicochemical properties of injectable oxaliplatin sustained-release microparticles

中文摘要英文摘要

目的:开发可注射奥沙利铂缓释微粒,并对其制备工艺和理化性质进行研究.方法:采用热熔挤出-冷冻研磨工艺制备可注射奥沙利铂缓释微粒,使用扫描电镜、粒度分析仪了解微粒形貌及粒径分布,采用液相色谱系统测量缓释微粒中奥沙利铂含量和微粒体外释放度.结果:可注射奥沙利铂缓释微粒粒度分布曲线稳定,微粒中奥沙利铂包封率为46.8%,包封率高;体外释放结果显示,奥沙利铂缓释微粒释放周期为144 h,最终释放度在80.0%以上,具有缓释性能;缓释微粒注射剂pH值在6.18~6.45的范围内,不会对注射部位造成损伤.结论:通过热熔挤出-冷冻研磨工艺制备的可注射奥沙利铂缓释微粒粒径分布均匀、药物包封率高,并且具有优异的缓控释特性以及稳定的理化性质.

Objective:Injectable oxaliplatin sustained-release microparticles were developed,and their preparation process and physical and chemical properties were studied.Methods:Injectable oxaliplatin sustained-release microparticles were prepared by hot melt extrusion freeze grinding process.The morphology and particle size distribution of the sustained-release microparticles were studied by scanning electron microscope and particle size analyzer.The content of oxaliplatin in the sustained-release mic-roparticles and the release of microsome were measured by liquid chromatography system.Results:The particle size distribution curve of injectable oxaliplatin sustained-release microparticles was stable,and the encapsulation efficiency of oxaliplatin in the mic-roparticles was 46.8%,which was high.The results of in vitro release showed that the release period of oxaliplatin sustained-re-lease microparticles was 144 hours,and the final release degree was above 80.0%,with sustained release performance.The pH value of the sustained-release microparticles injection is within the range of 6.18-6.45,and it will not cause damage to the injection site.Conclusion:Injectable oxaliplatin sustained-release microparticles prepared by hot melt extrusion freeze grinding process have uniform particle size distribution,high drug encapsulation efficiency,excellent slow and controlled release characteristics and sta-ble physical and chemical properties.

张俊伟;焦斌琪;曹坤;张彦志;陈铭哲;黄克祥;梁月祥;李井泉

海南医学院第一附属医院胃肠肿瘤外科,海南 海口 570100

化学工程

可注射奥沙利铂缓释微粒制备工艺理化性质

Injectable oxaliplatin sustained-release microparticlesPreparation processPhysical and chemical properties

《海南医学院学报》 2024 (010)

779-783 / 5

This study was supported by Key Research and Development Project of Hainan Provincial Science and Technology Department(ZDYF2020137) 海南省科学技术厅重点研发项目(ZDYF2020137)

10.13210/j.cnki.jhmu.20240023.002

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